4-Methylmorpholine → 2-(1-Benzothien-2-yl)-5-{[2-(1,3-thiazol-2-yl)butanoyl]amino}benzamide

HRID 503698ノート

反応式

HRID 503698 の反応式
[S:1]1[CH:5]=[CH:4][N:3]=[C:2]1C(C)C([O-])=O.[Na+].[S:12]1[C:16]2[CH:17]=[CH:18][CH:19]=[CH:20][C:15]=2[CH:14]=[C:13]1[C:21]1[CH:29]=[CH:28][C:27]([NH:30][C:31](=[O:36])[CH:32](Br)[CH2:33][CH3:34])=[CH:26][C:22]=1[C:23]([NH2:25])=[O:24].CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.CN1CCOCC1>CN(C=O)C>[S:12]1[C:16]2[CH:17]=[CH:18][CH:19]=[CH:20][C:15]=2[CH:14]=[C:13]1[C:21]1[CH:29]=[CH:28][C:27]([NH:30][C:31](=[O:36])[CH:32]([C:2]2[S:1][CH:5]=[CH:4][N:3]=2)[CH2:33][CH3:34])=[CH:26][C:22]=1[C:23]([NH2:25])=[O:24]

参加物

6

反応物 4

HCID 79724-MethylmorpholineHCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 594284882-(1-Benzothien-2-yl)-5-[(2-bromobutanoyl)amino]benzamideHCID 68691917HCID 68691917、化合物

生成物 1

HCID 594284902-(1-Benzothien-2-yl)-5-{[2-(1,3-thiazol-2-yl)butanoyl]amino}benzamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

Sodium 2-(2-thiazolyl)propionate (148 mg) is introduced into DMF (5 ml), and 2-(1-benzothien-2-yl)-5-[(2-bromobutanoyl)amino]benzamide (Example 8A; 171 mg), HATU (291 mg) and 4-methylmorpholine (194 mg) are added. The reaction mixture is stirred at RT overnight. The reaction mixture is concentrated and the residue is purified by preparative HPLC. 101 mg (36% of theory) of product are isolated.

後処理

  1. additionare added
  2. concentrationThe reaction mixture is concentrated
  3. customthe residue is purified by preparative HPLC
  4. custom101 mg (36% of theory) of product are isolated

出典と根拠

ORDレコード
ord-c4c998269c044ed584b44de529612a0f
出典データセット
uspto-grants-2010_08
特許番号
US07776922B2

反応ノート

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